Bioactivity | HPK1-IN-2 dihydrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity. HPK1-IN-2 dihydrochloride also inhibits Lck (0.05 µΜTarget |
IC50: <0.05 µΜ (HPK1); <0.05 µΜ (Flt3); 0.05-0.5 µΜ (Lck) |
Invitro |
In a-CD3 stimulated Jurkat E6. 1 cells, HPK1-IN-2 (example A1) inhibits SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 µΜ and >3µΜ, respectively[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HPK1-IN-2 dihydrochloride 相关抗体: |
In Vivo |
HPK1-IN-2 (example A1; 75-150 mg/kg; oral gavage; daily; for 21 days) treatment shows a dose-dependently tumor growth inhibition, with 75 mg/kg and 150 mg/kg QD inhibiting tumour growth by 44% and 64%, respectively[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS |
2375595-72-3 |
Formula |
C19H22Cl2N6OS |
Molar Mass |
453.39 |
Appearance |
固体 |
Transport |
Room temperature in continental US; may vary elsewhere. |
Storage |
4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) Reference |
[1]. Peter Brent Sampson, et al. Hpk1 inhibitors and methods of using same. WO2016205942A1. |
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